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. 2010 Nov 15;2:79–91. doi: 10.2147/BCTT.S5929

Table 1.

Review of the pharmacokinetics of lapatinib at the dose of 1250 mg/day, approved by the Food and Drug Administration

Absorption Oral, not available in IV form
 Tmax 3–4 hours
 Steady-state Cmax 2.43 μg/mL
 AUC 36.2 μg h/mL
Distribution Highly bound (>99%) to albumin
 Volume of distribution > 2200 L
Metabolism
 Primary CYP3A4 (70% of metabolism)
 Secondary CYP3A5, CYP2C19, CYP2C8
Elimination Primarily hepatic
 Single dose t1/2 14.2 hours
 Multiple doses t1/2 24 hours

Abbreviations: t1/2, elimination half-life; AUC, area under the concentration-time curve; IV, intravenous; Tmax, time to peak concentration; Cmax, maximum concentration.